Sivelestat (EI-546;LY-544349;ONO-5046) sodium is a potent, specific and competitive inhibitor of human neutrophil elastase with IC50 of 44 nM.
Sivelestat also inhibits leukocyte elastase obtained from rabbit, rat, hamster and mouse, does not inhibit trypsin, thrombin, plasmin, plasma kallikrein, pancreas kallikrein, chymotrypsin and cathepsin G (>10 uM).
Sivelestat attenuates LPS-induced acute lung inflammation in the hamster.
Physicochemical Properties
M.Wt
456.4447
Formula
C20H21N2NaO7S
Appearance
Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility
10 mM in DMSO
Chemical Name/SMILES
Propanoic acid, 2,2-dimethyl-, 4-[[[2-[[(carboxymethyl)amino]carbonyl]phenyl]amino]sulfonyl]phenyl ester, sodium salt (1:1)
References
1. Kawabata K, et al. Biochem Biophys Res Commun. 1991 Jun 14;177(2):814-20.
2. Yasui S, et al. Eur Respir J. 1995 Aug;8(8):1293-9.
3. Sakamaki F, et al. Am J Respir Crit Care Med. 1996 Jan;153(1):391-7.
